RPI-1是一种细胞渗透性，基于吲哚酮的ATP竞争性酪氨酸激酶抑制剂，已知靶向Ret，EGFR和Met。致瘤性，运动性和侵袭性增加已被描述为肿瘤细胞中HGF / Met失调的生物学结果，因此RPI-1处理H460细胞导致集落数和大小均大大降低。该化合物对小鼠NSCLC H460异种移植瘤和转移模型也具有活性。从机理上讲，RPI-1抑制Tyr1234 / Tyr1235的Met磷酸化，已知该蛋白会激活内在的激酶活性。 RPI-1 is a cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret, EGFR, and Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size. The compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 & MEN2A), but not H-Ras-, and transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met against Met in N592 in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592.
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RPI-1
Dangerous GoodsCAS number：269730-03-2 molecular formula：C17H15NO4
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compound introduction
Specs
| Chinese alias | 1,3-二氢-5,6-二甲氧基-3-[(4-羟苯基)亚甲基]-1H-吲哚-2-酮 | 3-(4-羟基苯亚甲基)-5,6-二甲氧基吲哚啉-2-酮 | ||
| English alias | RPI1 | RPI-1 | 2H-Indol-2-one, 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy- | HY-101246 | MFCD03852474 | 1,3-Dihydro-3-((4-hydroxyphenyl)methylene)-5,6-dimethoxy-2H-indol-2-one | RPI 1 | NCGC00480825-02 | (Z)-3-(4-hydroxybenzylidene)-5,6-dime | ||
| CAS number | 269730-03-2 | molecular formula | C17H15NO4 |
| molecular weight | 297.31 g/mol | Exact mass | ≥98% |
| PSA | 67.800 Ų | logp | 2.500 |
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Safety information
WGK Germany：
3
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dust mask type N95 (US)， Eyeshields， Gloves
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